2. Signaling Pathways
  3. Epigenetics
  4. Epigenetic Reader Domain
  5. BRD2 Isoform

BRD2

 

BRD2 Related Products (50):

Cat. No. Product Name Effect Purity
  • HY-100972
    ARV-771
    		Degrader 99.87%
    ARV-771 is a potent BET PROTAC based on E3 ligase von Hippel-Lindau with Kds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively.
  • HY-112090
    ABBV-744
    		Inhibitor 99.97%
    ABBV-744 is a first-in-class, orally active and selective inhibitor of the BDII domain of BET family proteins with IC50 values ranging from 4 to 18 nM for BRD2, BRD3, BRD4 and BRDT. ABBV-744 is primarily metabolized by CYP3A4 with agent-like properties enable the investigation of its antitumor efficacy and tolerability.
  • HY-136570
    GSK778
    		Inhibitor 99.14%
    GSK778 (iBET-BD1), a chemical probe, is a potent and selective BD1 bromodomain inhibitor of the BET proteins, with IC50s of 75 nM (BRD2 BD1), 41 nM (BRD3 BD1), 41 nM (BRD4 BD1), and 143 nM (BRDT BD1), respectively. GSK778 phenocopies the effects of pan-BET inhibitors in cancer models.
  • HY-162514
    BBC0403
    		Inhibitor 98.78%
    BBC0403 is a selective BRD2 inhibitor with Kds of 7.64 μM and 41.37 μM for BRD2 (BD2) and BRD2 (BD1), respectively. BBC0403 exhibitS higher binding specificity for BRD2 compared to BRD3 and BRD4. BBC0403 has the potential for osteoarthritis (OA) research.
  • HY-136571
    GSK046
    		Inhibitor 99.70%
    GSK046 (iBET-BD2), a chemical probe, is a potent, selective and orally active BD2 bromodomain inhibitor of the BET proteins, with IC50s of 264 nM (BRD2 BD2), 98 nM (BRD3 BD2), 49 nM (BRD4 BD2) and 214 nM (BRDT BD2), respectively. GSK046 has immunomodulatory activity.
  • HY-181003
    GSK785
    		Inhibitor
    GSK785 is a BRD2/4-selective, BRD3-sparing bivalent BET inhibitor. GSK785 inhibits production of the MCP1 cytokine in human whole blood. GSK785 can be used for the research of cancer.
  • HY-179589
    JQ-1 (carboxylic acid)-amine-PEG8-cyanogen
    		Degrader
    JQ-1 (carboxylic acid)-amine-PEG8-cyanogen is a Target Protein Ligand-Linker Conjugate that incorporates a ligand for BRD4 (HY-78695) and a PROTAC linker, which recruits E3 ligases. JQ-1 (carboxylic acid)-amine-PEG8-cyanogen can be used for the synthesis of PROTAC BET Degrader-14 (HY-179588 ).
  • HY-181735
    BET-IN-30
    		Inhibitor
    BET-IN-30 (Compound 11d) is a BTE family protein inhibitor, which can act as a BRD2/BRD3/BRD4 target protein ligand and be used for the synthesis of PROTACs, such as PROTAC BET Degrader-15 (HY-181729). BET-IN-30 exhibits potent anti-proliferative activity against acute myeloid leukemia (AML) cells such as MV4-11. BET-IN-30 can be used for the study of AML.
  • HY-141438
    SIM1
    		Inhibitor 99.47%
    SIM1 is a potent von Hippel-Lindau (VHL)-based trivalent PROTAC capable of degradation for all BET family members, with preference for BRD2 degradation (IC50=1.1 nM; Kd=186 nM). SIM1 shows sustained anti-cancer activity.
  • HY-160528
    IBG3
    		Inhibitor 98.53%
    IBG3 is a Molecular glue degrader targeting BRD2 and BRD4, with DC50 values of 8.6 pM and 6.7 pM, respectively. IBG3 binds simultaneously to the tandem bromodomains of BRD2/BRD4, induces intramolecular conformational changes, enhances the affinity of BRD2/BRD4 for DCAF16, and promotes ubiquitination and degradation. IBG3 is applicable to the research of chronic myeloid leukemia.
  • HY-138563
    GSK973
    		Inhibitor 99.97%
    GSK973, a chemical probe, is a highly selective, orally bioavailable inhibitor of the BD2s (second bromodomains) of the BET family, with a pIC50 of 7.8 and a pKd of 8.7 for BRD4 BD2. GSK973 displays a 1600-fold selectivity for BRD4 BD2 over BRD4 BD1. GSK973 shows good potency against BRD2 BD2, BRD3 BD2, and BRDT BD2 (pIC50=7.4~7.8; pKd=8.3~8.5).
  • HY-153385
    TMX1
    		Degrader 99.57%
    TMX1 is a covalent, selective BRD4 molecular glue degrader. TMX1 binds to the JQ1-binding site of BRD4BD2, forms covalent bonds with Cys58 of DCAF16 and Cys87 of GAK in a BRD4BD2-dependent template-assisted manner, stabilizes the BRD4-TMX1-DCAF16 ternary complex, and promotes the ubiquitination of BRD4 via the CRL4DCAF16 ubiquitin ligase complex. TMX1 induces selective degradation of BRD4, mild degradation of BRD2 and BRD3, as well as DCAF16-dependent cytotoxicity.
  • HY-153459
    IBG1
    		Degrader 99.88%
    IBG1 is a molecular glue degrader targeting BRD2 and BRD4 (DC50: 0.15 nM). IBG1 has no significant degradation effect on its paralogue BRD3. IBG1 can inhibit the growth of cancer cells and can be used in tumor research. (Pink: BRD2/BRD4 Ligand (HY-111139); Black: Linker; Blue: DCAF15 ligand-1 (HY-W037495)).
  • HY-101519
    BETd-260
    		Inhibitor 99.68%
    BETd-260 (ZBC 260) is a PROTAC connected by ligands for Cereblon and BET, with as low as 30 pM against BRD4 protein in RS4;11 leukemia cell line. BETd-260 potently suppresses cell viability and robustly induces apoptosis in hepatocellular carcinoma (HCC) cells.
  • HY-117286
    (S)-JQ-35
    		Inhibitor 99.46%
    (S)-JQ-35 (TEN-010) is an orally active, blood-brain barrier-permeable bromodomain inhibitor that selectively targets the bromodomain and extra-terminal domain (BET) protein family (BRD4, BRD3, BRD2 and BRDT). (S)-JQ-35 blocks the activation of Myc gene expression by BRD4, thereby inhibiting cancer cell proliferation and promoting cancer cell apoptosis. (S)-JQ-35 can be used in research related to NUT midline carcinoma and neuroblastoma.
  • HY-112429
    HJB97
    		Inhibitor 98.05%
    HJB97 is a high-affinity BET inhibitor with Ki values of 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), and 1.0 nM (BRD4 BD2). HJB97 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC BET degraders with antitumor activity. HJB97 can be used for the synthesis of BETd-260 (HY-101519).
  • HY-114504
    RVX-297
    		Inhibitor
    RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC50s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models.
  • HY-114416
    GS-626510
    		Inhibitor 99.46%
    GS-626510 is a potent, and orally active BET family bromodomains inhibitor, with Kd values of 0.59-3.2 nM for BRD2/3/4, with IC50 values of 83 nM and 78 nM foe BD1 and BD2, respectively.
  • HY-112610
    CF53
    		Inhibitor 99.81%
    CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM and an IC50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo.
  • HY-120000
    MS402
    		Inhibitor 98.36%
    MS402 is a BD1-selective BET BrD inhibitor with Kis of 77 nM, 718 nM, 110 nM, 200 nM, 83 nM, and 240 nM for BRD4(BD1), BRD4(BD2), BRD3(BD1), BRD3(BD2), BRD2(BD1) and BRD2(BD2), respectively. MS402 blocks Th17 cell differentiation and ameliorates colitis in mice.
Cat. No. Product Name / Synonyms Application Reactivity